Axelopran

Axelopran
Clinical data
ATC code
  • none
Identifiers
IUPAC name
  • 3-[(1R,5S)-8-[2-[cyclohexylmethyl-[(2S)-2,3-dihydroxypropanoyl]amino]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]benzamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC26H39N3O4
Molar mass457.615 g·mol−1
3D model (JSmol)
SMILES
  • C1CCC(CC1)CN(CCN2C3CCC2CC(C3)C4=CC=CC(=C4)C(=O)N)C(=O)C(CO)O
InChI
  • InChI=1S/C26H39N3O4/c27-25(32)20-8-4-7-19(13-20)21-14-22-9-10-23(15-21)29(22)12-11-28(26(33)24(31)17-30)16-18-5-2-1-3-6-18/h4,7-8,13,18,21-24,30-31H,1-3,5-6,9-12,14-17H2,(H2,27,32)/t21-,22+,23-,24-/m0/s1
  • Key:ATLYLVPZNWDJBW-KIHHCIJBSA-N

Axelopran (INN, USAN) (developmental code name TD-1211) is a drug which is under development by Theravance Biopharma for the treatment of opioid-induced constipation. It acts as a peripherally acting μ-opioid receptor antagonist and also acts on κ-, and δ-opioid receptors, with similar affinity for the μ- and κ-opioid receptors and about an order of magnitude lower affinity for the δ-opioid receptor. Axelopran has potent μ-opioid receptor antagonist activity on the gastrointestinal tract in vivo, and thus it produces a dose-dependent inhibition of opioid-induced delaying in gastric emptying in mice and rats following subcutaneous or oral administration.[1][2]

See also

References

  1. Armstrong SR, Campbell CB, Richardson CL, Vickery RG, Tsuruda PR, Long DD, et al. (June 2013). "The in vivo pharmacodynamics of the novel opioid receptor antagonist, TD-1211, in models of opioid-induced gastrointestinal and CNS activity". Naunyn-Schmiedeberg's Archives of Pharmacology. 386 (6): 471–8. doi:10.1007/s00210-013-0844-5. PMID 23512167. S2CID 15482326.
  2. Tsuruda PR, Vickery RG, Long DD, Armstrong SR, Beattie DT (June 2013). "The in vitro pharmacological profile of TD-1211, a neutral opioid receptor antagonist". Naunyn-Schmiedeberg's Archives of Pharmacology. 386 (6): 479–91. doi:10.1007/s00210-013-0850-7. PMID 23549670. S2CID 18963203.
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